- Kras inhibitory cyclic peptide compound
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The following were discovered: a cyclic peptide compound that interacts with Ras; and an unnatural amino acid that is useful in the production of said cyclic peptide compound. The cyclic peptide compound was also discovered to inhibit bonding between Ras and SOS. The following were additionally discovered: a specific unnatural amino acid included in said cyclic peptide compound; and a manufacturing method therefor.
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Paragraph 0682; 0830-0831
(2021/06/03)
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- N-HETERO-RING-SUBSTITUTED AMIDE DERIVATIVE
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Compounds are provided having an excellent hypoglycemic effect and β cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
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Paragraph 0049; 0050
(2014/06/24)
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- N-substituted 4-amino-3,3-dipropyl-2(3H)-furanones: New positive allosteric modulators of the GABAA receptor sharing electrophysiological properties with the anticonvulsant loreclezole
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1,4-Addition of benzylamine to 2(5H)-furanone followed by dialkylation of the 3-position with allylbromide gave (±)-4-benzyl-3,3-diallyl-2(3H)-furanone (8), which served as the intermediate for the synthesis of various N-substituted 4-amino-3,3-dipropyl-2
- El Hadri, Ahmed,Abouabdellah, Ahmed,Thomet, Urs,Baur, Roland,Furtmüller, Roman,Sigel, Erwin,Sieghart, Werner,Dodd, Robert H.
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p. 2824 - 2831
(2007/10/03)
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- Single Step Conversion of Chiral Carnitine and Derivatives into (S)- and (R)-β-Substituted-γ-Butyrolactones
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This paper describes an efficient single step transformation of chiral carnitine and carnitine derivatives into stereoisomerically pure (S)- and (R)-β-substituted-γ-butyrolactones, obtained by intramolecular nucleophilic displacement. (S)- Or (R)-carnitine and (R)-aminocarnitine inner salts give β-hydroxy-γ-butyrolactone and β-amino-γ-butyrolactone respectively (82% and 77%) with the same configuration as the starting material. (R)-Acetylaminocarnitine inner salt gives (R)-β-acetylamino-γ-butyrolactone (90%), while (R)-acetylcarnitine gives 2(5H)-furanone under the same reaction conditions (77%, via cyclization and subsequent elimination reaction). (R)-N-Benzyloxycarnitineamide gives a mixture of pyrrolidinone (11%) and furanoyl imidate (50%) derivatives. The direct transformation of waste (S)-carnitine into the valuable (S)-β-hydroxy-γ-butyrolactone or (after acetylation) into the precious 2(5H)-furanone is of particular interest.
- Calvisi, Giuseppina,Catini, Roberto,Chiariotti, Wilma,Giannessi, Fabio,Muck, Sandra,Tinti, Maria Ornella,De Angelis, Francesco
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